Flumequine-R-802-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEFlumequineCat. No.: HY-B0526CAS No.: 42835-25-6Synonyms: R-802分式: CHFNO分量: 261.25作靶點: Bacterial; Topoisomerase作通路: Anti-infection; Cell Cycle/DNA Damage儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體

2、外實驗 DMSO : 7.69 mg/mL (29.44 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.8278 mL 19.1388 mL 38.2775 mL5 mM 0.7656 mL 3.8278 mL 7.6555 mL10 mM 0.3828 mL 1.9139 mL 3.8278 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Flumequine (R-802)種喹諾酮類抗素，為拓撲異構(gòu)酶

3、II (Topoisomerase II) 抑制劑，IC50 值為 15 M(3.92 g/mL)。IC50 & Target Topoisomerase II15 M (IC50)1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Flumequine (R-802) is a topoisomerase II inhibitor, with an IC50 of 3.92 g/mL, and less potently inhibitsGyrase, with an IC50 of 1764 g/mL. Flumequine (0-6

4、25 g/mL) increases migration of nuclear DNA fromCHL cells 1. Flumequine (R-802) inhibits Spanish field isolates of B. hyodysenteriae with MIC50 and MIC90of 50 and 100 g/mL, and MBC50 and MBC90 of 50, 200 g/mL, respectively 2. Flumequine (R-802)suppresses A. salmonicida isolates with MIC ranging from

5、 0.06 to 32 g/mL 3.體內(nèi)研究 Flumequine (R-802) (0-500 mg/kg, p.o.) causes dose-related DNA damage in the stomach, colon, andurinary bladder of mice, 1 and 3 h but not 24 h after its administration 1.PROTOCOLCell Assay 1 The Chinese hamster lung cell line CHL/IU is routinely maintained in monolayer cultu

6、re in Dulbeccosmodified MEM medium supplemented with 10% fetal bovine serum at 37C under a 5% CO2 atmosphere.Exponentially growing cells are treated with Flumequine (R-802) dissolved in DMSO for 1 h. The dose rangeis chosen in order to obtain both damaged and highly damaged cells. Following Flumequi

7、ne (R-802)treatment, cells are embedded in GP42 agarose dissolved in saline at 1%. Cell number and cell viability aredetermined for each dose 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Infant and young-adult male ddY mice at 4 and 7 weeks

8、of age, respectively, are used after 1 week ofAdministration 1 acclimatization. Groups are treated once orally with Flumequine (R-802) at . Adult mice are sacrificed at 3and 24 h after treatment, and 8 organs, the stomach, colon, liver, kidney, urinary bladder, lung, brain, andbone marrow, are remov

9、ed. Infant mice are sacrificed 3 and 24 h after treatment, and the livers are excised.In another study, the genotoxicity of Flumequine (R-802) is studied in the regenerating liver of adult mice. Forthis purpose, male mice at 8 weeks-of-age are anesthetized with ether and 3 major lobes of the liver,

10、leftlateral lobe, left medial lobe, and right lateral lobe, are removed. Four days after the hepatectomy, mice aresubjected to oral administration of Flumequine (R-802) once. They are sacrificed 3 h after FL-treatment andregenerated livers are sampled. Slides for the comet assay are prepared at each

11、 set time 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Chemosphere. 2019 Mar. J Mol Med (Berl). 2019 Jun 14.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Kashida Y, et al. Mechanistic study on flumequine hepatoca

12、rcinogenicity focusing on DNA damage in mice. Toxicol Sci. 2002Oct;69(2):317-21.2. Aller-Morn LM, et al. Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriae. Res Vet Sci.2015 Dec;103:51-3.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. Giraud E, et al. Mechanisms of quinolone resistance and clonal relationship among Aeromonas salmonicida strains isolated from rearedfish with furunculosis. J Med Microbiol. 2004 Sep;53(Pt 9):895-901.McePdfHeight